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Cu-Catalyzed Intramolecular Amidation of Unactivated C(sp(3))-H Bonds To Synthesize N-Substituted Indolines

机译:铜催化的未激活的C(sp(3))-H键的分子内酰胺化合成N-取代的二氢吲哚

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摘要

A copper-catalyzed intramolecular amidation of unactivated C(sp(3))-H bonds to construct indoline derivatives has been developed. Such an amidation proceeded well at primary C-H bonds preferred to secondary C-H bonds. The transformation owned a broad substrate scope. The corresponding indolines were obtained in good to excellent yields. N-Formal and other carbonyl groups were suitable and were easily deprotected and transformed into methyl or long-chained alkyl groups. Preliminary mechanistic studies suggested a radical pathway.
机译:铜催化分子内酰胺化的未激活的C(sp(3))-H键来构造吲哚啉衍生物。这样的酰胺化在优选于仲C-H键的伯C-H键处进行得很好。转型拥有广阔的基础范围。获得了相应的二氢吲哚,收率为好至极好。 N-甲醛和其他羰基是合适的,并且容易脱保护并转化为甲基或长链烷基。初步的力学研究表明了一个根本途径。

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